In 2013,Suzuki, Kenji; Hamada, Yoshio; Nguyen, Jeffrey-Tri; Kiso, Yoshiaki published 《Novel BACE1 inhibitors with a non-acidic heterocycle at the P1′ position》.Bioorganic & Medicinal Chemistry published the findings.Name: 5-Bromothiazol-2-amine The information in the text is summarized as follows:
We have reported potent peptidic and non-peptidic BACE1 inhibitors with a hydroxymethylcarbonyl (HMC) isostere as a substrate transition-state mimic. However, our potent inhibitors possess a tetrazole ring at the P1′ position. It is desirable that central nervous system (CNS) drugs do not possess an acidic moiety. In this study, we synthesized non-acidic BACE1 inhibitors with heterocyclic derivatives at the P1′ position. KMI-1764 I exhibited potent inhibitory activity (IC50 = 27 nM). Interestingly, these non-acidic inhibitors tended to follow the quant. structure-activity relationship (QSAR) equation and interacted with BACE1-Arg235 in the binding model. The experimental process involved the reaction of 5-Bromothiazol-2-amine(cas: 3034-22-8Name: 5-Bromothiazol-2-amine)
5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Name: 5-Bromothiazol-2-amine
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica